Combination of a selective ppar-gamma modulator and an incretin for the treatment of diabetes and obesity

Abstract

The present invention relates to pharmaceutical compositions and methods for the treatment of diabetes, obesity or disorders related to diabetes or obesity. The compositions comprise a combination of a selective PPARγ modulator and an incretin. The methods include the administration of the combination of a selective PPARγ modulator and an incretin.

Description

1. FIELD OF THE INVENTION[0001]The present invention relates to combinations of a selective PPARγ (PPAR-gamma) modulator and an incretin, pharmaceutical compositions and kits containing such combinations, and methods of using such combinations for the treatment of diabetes, pre-diabetes and obesity and / or disorders related to diabetes, pre-diabetes or obesity.2. BACKGROUND OF THE INVENTION[0002]Diabetes is now considered to be a worldwide epidemic. Globally, the number of people with diabetes is expected to rise from the current estimate of 150 million to 220 million in 2010 and 300 million in 2025. In the United States, it is estimated that as of 2002, 18.2 million people (6.3% of the total population) were diabetic.[0003]Diabetes refers to a disease process derived from multiple causative factors and characterized by elevated levels of plasma glucose or hyperglycemia in the fasting state or after administration of glucose during an oral glucose tolerance test. Persistent or uncont...

AI Technical Summary

Benefits of technology

"The present invention provides combinations of a selective PPARγ modulator and an incretin for the treatment of diabetes, obesity, or related disorders. These combinations have clinical advantages over using a single agent alone, including increased efficacy and reduction of side effects. The selective PPARγ modulator is compound 101 of formula I or a pharmaceutically acceptable salt, hydrate, or polymorph thereof. The incretin can be a GLP-1 receptor agonist or a GIP receptor agonist, such as exenatide, liraglutide, taspoglutide, CJC-1131, LY307161 SR, or AVE0010 / ZP10. The combinations are useful for treating disorders related to diabetes or obesity, such as hyperglycemia, prediabetes, impaired glucose tolerance, impaired fasting glucose, dyslipidemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, high LDL levels, atherosclerosis, hypertension, sleep apnea, polycystic ovarian syndrome, and metabolic syndrome. The invention also provides methods of treating these disorders by administering the compound of formula (I) and an incretin. The invention also provides pharmaceutical compositions and kits containing the compound of formula (I) and an incretin."

Problems solved by technology

Persistent or uncontrolled hyperglycemia is associated with increased and premature morbidity and mortality and thus presents significant public health concerns.

While physical exercise and reductions in dietary intake of calories will dramatically improve the diabetic condition, compliance with this treatment is very poor because of well-entrenched sedentary lifestyles and excess food consumption, especially of foods containing high amounts of saturated fat.

However, dangerously low levels of plasma glucose can result from administration of insulin or insulin secretagogues (sulfonylureas or meglitinide), and an increased level of insulin resistance due to the even higher plasma insulin levels can occur.

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